1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

Irbinitinib (Synonyms: ARRY-380; ONT-380)

Cat. No.: HY-16069 Purity: 99.57%
Handling Instructions

Irbinitinib (ARRY-380; ONT-380) is a potent and selective HER2 inhibitor with an IC50 of 8 nM.

For research use only. We do not sell to patients.
Irbinitinib Chemical Structure

Irbinitinib Chemical Structure

CAS No. : 937263-43-9

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10 mM * 1 mL in DMSO USD 79 In-stock
5 mg USD 72 In-stock
10 mg USD 108 In-stock
50 mg USD 288 In-stock
100 mg USD 528 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Irbinitinib (ARRY-380; ONT-380) is a potent and selective HER2 inhibitor with an IC50 of 8 nM.

IC50 & Target

IC50: 8 nM (HER2)[1]

In Vitro

ONT-380 (ARRY-380) is a potent, selective, ATP-competitive, orally administered small-molecule inhibitor of HER2. ONT-380 has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. ONT-380 (ARRY-380) selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR. In HER2 overexpressing cell lines, ONT-380 blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt. By contrast, in the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that ONT-380 may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition[1].

In Vivo

In preclinical studies with intracranial tumor models, treatment of mice with ONT-380 compared with lapatinib or neratinib shows a survival benefit when each drug is dosed at the maximum-tolerated dose[1]. In the ARRY-380-treated-group, 75% of the animals are alive on Day 43. ARRY-380 and its active metabolite causes a significant reduction in brain pErbB2 (80%)[2]. ARRY-380 demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. ARRY-380 (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions. At dose of 100 mg/kg/d of ARRY-380 in combination with trastuzumab, there is 100% TGI and all animals have complete responses[3].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0811 mL 10.4054 mL 20.8108 mL
5 mM 0.4162 mL 2.0811 mL 4.1622 mL
10 mM 0.2081 mL 1.0405 mL 2.0811 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[3]

Mice: For the SKOV-3 tumor studies, female nude mice are inoculated with cells subcutaneously in the flank. Animals received: doses of ARRY-380 ranging up to 200 mg/kg/d, PO; and/or trastuzumab at 20 mg/kg, IP, Q3D or QW; and/or docetaxel at 10 mg/kg, IV, Q3D; and/or bevacizumab at 10 mg/kg, IP, Q4D x3. Tumor size is measured at regular intervals and subsets of animals are monitored for up to 90 days to determine tumor-free survival[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

480.52

Formula

C₂₆H₂₄N₈O₂

CAS No.

937263-43-9

SMILES

CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.57%

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Irbinitinib
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